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One-Step Preparation of Poly-Lactic-Co-Glycolic-Acid Microparticles to Prevent the Initial Burst Release of Encapsulated Water-Soluble Proteins

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DOI: 10.4236/pp.2013.48083    4,111 Downloads   6,268 Views   Citations


An initial burst is often observed during the release of active pharmaceutical ingredients (APIs) from poly-lactic-coglycolic-acid (PLGA) microparticles (MPs) which have been prepared by the emulsion-solvent evaporation method. Herein, we describe the development of a simple one-step coating method that suppresses the initial burst release process. This new method involves coating the PLGA-MPs with PLGA, with the coating process being performed through the phase separation of PLGA on the surface of PLGA-MPs using the emulsion-solvent evaporation method. Bovine serum albumin (BSA) was encapsulated in the PLGA-MPs as a model API. The coated MPs were spherical in shape with no pores on their smooth surface, whereas the non-coated PLGA-MPs had porous surfaces. An in vitro release study showed that the residual levels of BSA in the coated and non-coated PLGA-MPs after 1 h were about 99% and 16% of the original loads, respectively. The one-step coating method therefore represents a useful method for preparing PLGA-MPs that do not give an initial burst release of proteinaceous APIs.

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H. Takabe, M. Ohkuma, Y. Iwao, S. Noguchi and S. Itai, "One-Step Preparation of Poly-Lactic-Co-Glycolic-Acid Microparticles to Prevent the Initial Burst Release of Encapsulated Water-Soluble Proteins," Pharmacology & Pharmacy, Vol. 4 No. 8, 2013, pp. 578-583. doi: 10.4236/pp.2013.48083.

Conflicts of Interest

The authors declare no conflicts of interest.


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